EP2813215A4 - 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol lipid microsphere preparation and preparation method therefor - Google Patents

2,2',6,6'-tetraisopropyl-4,4'-2-biphenol lipid microsphere preparation and preparation method therefor

Info

Publication number
EP2813215A4
EP2813215A4 EP12868324.0A EP12868324A EP2813215A4 EP 2813215 A4 EP2813215 A4 EP 2813215A4 EP 12868324 A EP12868324 A EP 12868324A EP 2813215 A4 EP2813215 A4 EP 2813215A4
Authority
EP
European Patent Office
Prior art keywords
preparation
tetraisopropyl
method therefor
lipid microsphere
biphenol lipid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP12868324.0A
Other languages
German (de)
French (fr)
Other versions
EP2813215A1 (en
EP2813215B1 (en
Inventor
Rutao Wang
Tao Chen
Shupan Guo
Huijing Hu
Long An
Weijiao Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
XI'AN LIBANG PHARMACEUTICAL CO Ltd
XI AN LIBANG PHARMACEUTICAL CO Ltd
Original Assignee
XI'AN LIBANG PHARMACEUTICAL CO Ltd
XI AN LIBANG PHARMACEUTICAL CO Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by XI'AN LIBANG PHARMACEUTICAL CO Ltd, XI AN LIBANG PHARMACEUTICAL CO Ltd filed Critical XI'AN LIBANG PHARMACEUTICAL CO Ltd
Publication of EP2813215A1 publication Critical patent/EP2813215A1/en
Publication of EP2813215A4 publication Critical patent/EP2813215A4/en
Application granted granted Critical
Publication of EP2813215B1 publication Critical patent/EP2813215B1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5089—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Manufacturing Of Micro-Capsules (AREA)
EP12868324.0A 2012-02-06 2012-03-07 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol lipid microsphere preparation and preparation method therefor Active EP2813215B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2012100256112A CN102525921B (en) 2012-02-06 2012-02-06 2,2',6,6'-tetraisopropyl-4,4'-bigeminy phenol lipid microsphere preparation and preparation method thereof
PCT/CN2012/072031 WO2013117022A1 (en) 2012-02-06 2012-03-07 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol lipid microsphere preparation and preparation method therefor

Publications (3)

Publication Number Publication Date
EP2813215A1 EP2813215A1 (en) 2014-12-17
EP2813215A4 true EP2813215A4 (en) 2015-07-08
EP2813215B1 EP2813215B1 (en) 2016-07-13

Family

ID=46334755

Family Applications (1)

Application Number Title Priority Date Filing Date
EP12868324.0A Active EP2813215B1 (en) 2012-02-06 2012-03-07 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol lipid microsphere preparation and preparation method therefor

Country Status (6)

Country Link
US (2) US20140370101A1 (en)
EP (1) EP2813215B1 (en)
JP (1) JP5748926B2 (en)
CN (1) CN102525921B (en)
CA (1) CA2865777C (en)
WO (1) WO2013117022A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102525921B (en) 2012-02-06 2013-08-07 西安力邦制药有限公司 2,2',6,6'-tetraisopropyl-4,4'-bigeminy phenol lipid microsphere preparation and preparation method thereof
CN104557532B (en) * 2015-01-13 2017-03-01 西安力邦制药有限公司 Bigeminy benzene derivative and its application
CN104546809B (en) * 2015-01-13 2018-08-24 西安力邦制药有限公司 Application of 3,3 ', 5,5 '-tetra isopropyls-the 4,4 '-bigeminy phenol in preventing and treating cerebral arterial thrombosis
CN112336868A (en) * 2020-10-28 2021-02-09 西安力邦医美科技有限公司 Polyethylenimine matrine lipid microsphere antifungal preparation and application thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040225022A1 (en) * 2003-05-09 2004-11-11 Desai Neil P. Propofol formulation containing reduced oil and surfactants
WO2007052288A2 (en) * 2005-08-05 2007-05-10 Bharat Serums & Vaccines Ltd. Intravenous propofol emulsion compositions having preservative efficacy

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9405593D0 (en) * 1994-03-22 1994-05-11 Zeneca Ltd Pharmaceutical compositions
GB9514878D0 (en) * 1995-07-20 1995-09-20 Danbiosyst Uk Vitamin E as a solubilizer for drugs contained in lipid vehicles
IN186588B (en) * 1999-07-28 2001-10-06 Vinod Daftary Gautam Dr
SE0001865D0 (en) * 2000-05-19 2000-05-19 Astrazeneca Ab Management of septic shock
IN188924B (en) * 2001-03-01 2002-11-23 Bharat Serums & Vaccines Ltd
US20060148776A1 (en) * 2003-03-13 2006-07-06 Conforma Therapeutics Corporation Drug formulations having long and medium chain triglycerides
CN1478465A (en) * 2003-07-14 2004-03-03 丽 佟 Biphenyl diester liquid medicinal composition containing fat
US20050255154A1 (en) * 2004-05-11 2005-11-17 Lena Pereswetoff-Morath Method and composition for treating rhinitis
WO2008023384A1 (en) * 2006-08-24 2008-02-28 Bharat Serums & Vaccines Ltd. Propofol emulsion compositions for intravenous administration
CN101804043B (en) * 2010-04-30 2012-04-11 西安力邦制药有限公司 Application of 2-phenylphenol and derivatives thereof to medicine for treating epilepsia
CN101940549B (en) * 2010-08-27 2012-04-25 北京中海康医药科技发展有限公司 Flurbiprofen axetil medium-chain and long-chain fat emulsion and preparation method thereof
CN102525921B (en) 2012-02-06 2013-08-07 西安力邦制药有限公司 2,2',6,6'-tetraisopropyl-4,4'-bigeminy phenol lipid microsphere preparation and preparation method thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040225022A1 (en) * 2003-05-09 2004-11-11 Desai Neil P. Propofol formulation containing reduced oil and surfactants
WO2007052288A2 (en) * 2005-08-05 2007-05-10 Bharat Serums & Vaccines Ltd. Intravenous propofol emulsion compositions having preservative efficacy

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
OGATA M. ET AL.: "Solubilization of dipropofol, an antibacterial agent, using saccharide and ascorbic acid", BIOL. PHARM. BULL., vol. 30, no. 8, August 2007 (2007-08-01), pages 1565 - 1568, XP002739972 *
See also references of WO2013117022A1 *

Also Published As

Publication number Publication date
EP2813215A1 (en) 2014-12-17
US10154967B2 (en) 2018-12-18
EP2813215B1 (en) 2016-07-13
CN102525921A (en) 2012-07-04
JP5748926B2 (en) 2015-07-15
JP2015506378A (en) 2015-03-02
WO2013117022A1 (en) 2013-08-15
CN102525921B (en) 2013-08-07
US20160235684A1 (en) 2016-08-18
CA2865777C (en) 2015-09-22
US20140370101A1 (en) 2014-12-18
CA2865777A1 (en) 2013-08-15

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